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    • 74. 发明申请
    • TRICYCLIC RADIOLABELED D4 RECEPTOR LIGANDS
    • WO1998001164A1
    • 1998-01-15
    • PCT/CA1997000465
    • 1997-06-30
    • RESOLUTION PHARMACEUTICALS INC.
    • RESOLUTION PHARMACEUTICALS INC.POLLAK, AlfredDUNN-DUFAULT, Robert
    • A61K51/04
    • C07D337/14A61K51/0459A61K2123/00C07D223/20C07D243/38C07D267/20C07D281/16C07D313/14
    • Herein described are radiolabeled compounds useful to image D4 receptors in vivo, of formula (I), wherein X is selected from NH, O and S; X is selected from CH and N; Z is selected from iodide, cyano, nitro, tri(loweralkyl)tin and a radioisotopic iodide; and R is selected from H, lower alkyl, piperonyl, C1-4alkenyl, C1-4alkynyl and C1-4alkenyl substituted with one of iodide, tri(loweralkyl)tin and radioisotopic iodide; with the provisos that: (1) when one of Z and R is radioisotopic, the other of Z and R is not or does not incorporate iodide; and (2) when one of Z and R is or incorporates tri(loweralkyl)tin, the other of Z and R is not or does not incorporate iodide or radioisotopically labeled iodide. The radiopharmaceutical compounds are useful particularly to image localisation of D4 receptor in the human brain, and can therefore aid in the diagnosis of schizophenia and other medical conditions in which the D4 receptor is implicated.
    • 本文描述的是用于在体内对D4受体(式(I))进行成像的放射性标记的化合物,其中X 1选自NH,O和S; X 2选自CH和N; Z选自碘化物,氰基,硝基,三(低级烷基)锡和放射性同位素碘化物; 和R 1选自H,低级烷基,胡椒基,C 1-4烯基,C 1-4炔基和被碘,三(低级烷基)锡和放射性同位素碘化物之一取代的C 1-4链烯基; 条件是:(1)当Z和R 1中的一个是放射性同位素时,Z和R 1中的另一个不是或不包含碘化物; 和(2)当Z和R 1中的一个为或并入三(低级烷基)锡时,Z和R 1中的另一个不是或不包含碘化物或放射性同位素标记的碘化物。 放射性药物化合物特别用于人类脑中D4受体的图像定位,因此可以有助于诊断分裂症和其它D4受体的其他医学病症。